Discovery of novel anti-diabetic drugs by targeting lipid metabolism

Xiu Zhou, Jun Xu, Yuguang Shi, Ji Ming Ye

Research output: Contribution to journalArticlepeer-review

12 Scopus citations


Accumulation of toxic lipids is the most common etiology of insulin resistance in type 2 diabetes and associated metabolic disorders such as obesity and non-alcoholic fatty liver disease. Understanding of the underlying mechanisms has revealed various opportunities to target key regulators in lipid metabolic pathways for the treatment of metabolic diseases. Here, we review the discovery and development of potential anti-diabetic drugs with primary effects on cellular targets leading to reductions of intracellular lipids in key organs. We will particularly focus on AMPK, SIRT1, PGC-1α, SREBP-1c, ChREBP, ACC, PPARs and HSPs which either stimulate in fatty acid oxidation (energy expenditure) or inhibit de novo lipogenesis.

Original languageEnglish (US)
Pages (from-to)1372-1380
Number of pages9
JournalCurrent drug targets
Issue number12
StatePublished - Nov 1 2015
Externally publishedYes


  • Anti-diabetic drug targets
  • Drug discovery
  • Insulin resistance
  • Lipid metabolism

ASJC Scopus subject areas

  • Drug Discovery
  • Molecular Medicine
  • Clinical Biochemistry
  • Pharmacology


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